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公开(公告)号：US5883129A
公开(公告)日：1999-03-16
申请号：US433337
申请日：1995-05-04
申请人： Susanna Karin Maria Bjork , Birgitta Kristina Gotthammar , Mats Torbjorn Linderberg , Johan Per Luthman , Kerstin Margareta Irma Persson , Robert Schwarcz , Barry K. Carpenter
发明人： Susanna Karin Maria Bjork , Birgitta Kristina Gotthammar , Mats Torbjorn Linderberg , Johan Per Luthman , Kerstin Margareta Irma Persson , Robert Schwarcz , Barry K. Carpenter
IPC分类号： A61K31/195 , A61P25/00 , A61P25/08 , A61P25/28 , A61P43/00 , C07C45/27 , C07C47/277 , C07C205/37 , C07C205/59 , C07C205/60 , C07C227/04 , C07C229/64 , C07C255/57 , C07C255/59 , C07C303/30 , C07C309/77 , C07C319/12 , C07C323/62 , C07D333/20 , A61K31/19 , A61K31/24 , C07C229/00 , C07C229/52
CPC分类号： C07D333/20 , C07C205/37 , C07C205/59 , C07C205/60 , C07C229/64 , C07C45/27 , C07C47/277
摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OCF.sub.3 and SCF.sub.3 with the proviso that the compound of formula I wherein R.sub.1 and R.sup.2 =H, X=Br and Y=Me is excluded;or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxyanthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.
摘要翻译： PCT No.PCT / SE94 / 00153 Sec。 371日期：1995年5月4日 102（e）日期1995年5月4日PCT提交1995年2月24日PCT公布。 公开号WO94 / 19316 PCT 1994年9月1日，本发明涉及通式Ⅰ的3-羟基邻氨基苯甲酸3-HANA的新型衍生物，其中R1和R2相同或不同，选自H和烷基; X和Y相同或不同，选自烷氧基，芳氧基，烷基，烷硫基，芳硫基，氟烷基，卤素，氰基，OCF 3和SCF 3，条件是其中R 1和R 2 = H，X = Br和 Y = Me被排除; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责内源性神经毒素喹啉酸QUIN的3-羟基邻氨基苯甲酸酶加氧酶3-HAO的用途。
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公开(公告)号：US5688945A
公开(公告)日：1997-11-18
申请号：US770488
申请日：1996-12-20
申请人： Susanna Karin Maria Bjork , Birgitta Kristina Gotthammar , Mats Torbjorn Linderberg , Johan Per Luthman , Kerstin Margareta Irma Persson , Robert Schwarcz
发明人： Susanna Karin Maria Bjork , Birgitta Kristina Gotthammar , Mats Torbjorn Linderberg , Johan Per Luthman , Kerstin Margareta Irma Persson , Robert Schwarcz
IPC分类号： C07D333/04 , A61K31/195 , A61K31/196 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P9/10 , A61P25/00 , A61P43/00 , C07C205/26 , C07C205/37 , C07C205/59 , C07C227/04 , C07C227/16 , C07C227/18 , C07C229/64 , C07C229/70 , C07C253/30 , C07C255/57 , C07C255/59 , C07C315/04 , C07C317/46 , C07C317/48 , C07C319/20 , C07C323/62 , C07C323/63 , C07D307/34 , C07F7/12 , C07D227/02 , C07C315/00 , C07C317/00
CPC分类号： C07C205/59 , C07C205/26 , C07C205/37 , C07C229/64 , C07C229/70 , C07C255/59 , C07C2102/10
摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.7 =H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.
摘要翻译： 本发明涉及通式Ⅰ的3-羟基邻氨基苯甲酸的新型衍生物，3-HANA，其中R 1和R 2相同或不同并且选自H和烷基; X选自烷硫基，芳硫基，芳氧基，卤素和氰基; R 3，R 4相同或不同，选自卤素，甲基，氟烷基，氰基和Z-R 5，其中Z选自CH n，NH m，O，S，SO 2和CO，其中n = 1或2; m = 0或1，R 5选自烷基，芳基和氟烷基; 或R3和R4一起形成饱和或不饱和的环系YVZ，其中Y和Z彼此独立地如上述Z所定义，V选自C 1 -C 3亚烷基或亚烯基-N =，-N = N- 和＆lt; IMAGE＆gt;其中R7 = H或烷基; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责产生内源性神经毒素喹啉酸QUIN的3-羟基 - 邻氨基苯甲酸加氧酶3-HAO的用途。
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公开(公告)号：US5661183A
公开(公告)日：1997-08-26
申请号：US433339
申请日：1995-05-04
申请人： Susanna Karin Maria Bjork , Birgitta Kristina Gotthammar , Mats Torbjorn Linderberg , Johan Per Luthman , Kerstin Margareta Irma Persson , Robert Schwarcz
发明人： Susanna Karin Maria Bjork , Birgitta Kristina Gotthammar , Mats Torbjorn Linderberg , Johan Per Luthman , Kerstin Margareta Irma Persson , Robert Schwarcz
IPC分类号： C07D333/04 , A61K31/195 , A61K31/196 , A61K31/275 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61P9/10 , A61P25/00 , A61P43/00 , C07C205/26 , C07C205/37 , C07C205/59 , C07C227/04 , C07C227/16 , C07C227/18 , C07C229/64 , C07C229/70 , C07C253/30 , C07C255/57 , C07C255/59 , C07C315/04 , C07C317/46 , C07C317/48 , C07C319/20 , C07C323/62 , C07C323/63 , C07D307/34 , C07F7/12 , C07C229/00
CPC分类号： C07C205/59 , C07C205/26 , C07C205/37 , C07C229/64 , C07C229/70 , C07C255/59 , C07C2102/10
摘要： The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA of general formula (I), wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z-R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y-V-Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and (a), wherein R.sub.7 .dbd.H or alkyl; or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxy-anthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.
摘要翻译： PCT No.PCT / SE94 / 00152 Sec。 371日期：1995年5月4日 102（e）日期1995年5月4日PCT 1994年2月22日提交PCT公布。 公开号WO94 / 19315 （I）本发明涉及3-羟基邻氨基苯甲酸的新型衍生物，通式（I）的3-HANA，其中R 1和R 2相同或不同并选自H和烷基 ; X选自烷硫基，芳硫基，芳氧基，卤素和氰基; R 3，R 4相同或不同，选自卤素，甲基，氟烷基，氰基和Z-R 5，其中Z选自CH n，NH m，O，S，SO 2和CO，其中n = 1或2; m = 0或1，R 5选自烷基，芳基和氟烷基; 或R3和R4一起形成饱和或不饱和的环系YVZ，其中Y和Z彼此独立地如上述Z所定义，V选自C 1 -C 3亚烷基或亚烯基-N =，-N = N- 和（a），其中R7 = H或烷基; 或其药学上可接受的盐，其制备方法和中间体，新型药物组合物及其用于抑制负责产生内源性神经毒素喹啉酸QUIN的3-羟基 - 邻氨基苯甲酸加氧酶3-HAO的用途。
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